Onyx Therapeutics, Inc.

Tony Muchamuel

Christopher J Kirk

Jing Jiang

Naveen Bejugam

Katherine A Chu

Mouhannad Jumaa

Zhengping Wang

Jeffrey Joseph Jones

Elena T Chan

Hansen Wong

Rahul Vishram Manek

Ying Fang

Sanjeev Sharma

Mouhannad Jamaa

Liposomal compositions comprising peptide epoxyketone compounds are described, as well as methods of making and using such liposomal compositions. These liposomal compositions enhance the therapeutic window of peptide epoxyketone compounds by improving in vivo half-life relative to non-liposomal compositions comprising peptide epoxyketone compounds, providing desirable pharmacodynamic profiles, and providing anti-tumor activity in a human tumor xenograft model, greater than or equal to non-liposomal compositions comprising peptide epoxyketone compounds. Further, experiments performed in support of the present invention demonstrated improved tolerability of liposomal compositions comprising peptide epoxyketone compounds.

Liposomal compositions of epoxyketone-based proteasome inhibitors

This disclosure features modified release pharmaceutical formulations (e.g., extended release pharmaceutical formulations; e.g., solid dosage forms, e.g., tablets) that are useful for the oral administration of oprozomib, or a pharmaceutically acceptable salt thereof, to a human or animal subject as well as methods of making and using the formulations.

Modified release formulations for oprozomib

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Boulder Creek, CA, United States of America

Tony Muchamuel